US11912685B2ActiveUtilityA1

Biphenyl diaryl pyrimidine derivative with aromatic heterocyclic structure

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Assignee: UNIV FUDANPriority: Mar 8, 2021Filed: Sep 7, 2021Granted: Feb 27, 2024
Est. expiryMar 8, 2041(~14.7 yrs left)· nominal 20-yr term from priority
C07D 401/12A61P 31/18C07D 239/48C07D 401/14C07D 403/12C07D 405/12C07D 409/12
56
PatentIndex Score
0
Cited by
3
References
7
Claims

Abstract

This application provides a biphenyl diaryl pyrimidine derivative with an aromatic heterocyclic structure, a pharmaceutically-acceptable salt, a stereoisomer, a hydrate and a solvate thereof, where the biphenyl diaryl pyrimidine derivative is shown in formula (I). This application also provides a pharmaceutical composition containing the biphenyl diaryl pyrimidine derivative, or a pharmaceutically-acceptable salt, a stereoisomer, a hydrate and a solvate thereof, and a pharmaceutically-acceptable carrier. This application further provides a method of treating AIDS by administering a therapeutically effective amount of the pharmaceutical composition to a patient in need.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       1. A compound of formula (I), or a pharmaceutically-acceptable salt, a stereoisomer, a hydrate or a solvate thereof: 
       
         
           
           
               
               
           
         
         wherein R 1  is selected from the group consisting of substituted and unsubstituted furyl, substituted and unsubstituted thienyl, substituted and unsubstituted pyrazolyl, substituted and unsubstituted imidazolyl, substituted and unsubstituted thiazolyl, substituted and unsubstituted pyridyl, substituted and unsubstituted pyrimidinyl, substituted and unsubstituted p-aminophenyl and substituted and unsubstituted C 7 -C 10  aromatic heterocyclic group. 
       
     
     
       2. The compound of  claim 1 , or a pharmaceutically-acceptable salt, a stereoisomer, a hydrate or a solvate thereof, wherein the compound is selected from the group consisting of: 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
       3. The compound of  claim 1 , or a pharmaceutically-acceptable salt, a stereoisomer, a hydrate or a solvate thereof, wherein the pharmaceutically-acceptable salt is selected from the group consisting of hydrochloride, hydrobromide, formate, methanesulfonate, trifluoromethanesulfonate, sulfate, phosphate, acetate, p-toluenesulfonate, tartrate, citrate, succinate, maleate, fumarate and malate. 
     
     
       4. A pharmaceutical composition, comprising a pharmaceutically effective amount of the compound of  claim 1 , or a pharmaceutically-acceptable salt, a stereoisomer, a hydrate or a solvate thereof, and a pharmaceutically-acceptable carrier. 
     
     
       5. A compound of formula (I), or a polycrystal, a eutectic or a single-enantiomer X-ray diffraction single crystal thereof: 
       
         
           
           
               
               
           
         
         wherein R 1  is selected from the group consisting of substituted and unsubstituted furyl, substituted and unsubstituted thienyl, substituted and unsubstituted pyrazolyl, substituted and unsubstituted imidazolyl, substituted and unsubstituted thiazolyl, substituted and unsubstituted pyridyl, substituted and unsubstituted pyrimidinyl, substituted and unsubstituted p-aminophenyl and substituted and unsubstituted C 7 -C 10  aromatic heterocyclic group. 
       
     
     
       6. The compound of  claim 5 , or a polycrystal, a eutectic or a single-enantiomer X-ray diffraction single crystal thereof, wherein the compound is selected from the group consisting of: 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
       7. A pharmaceutical composition, comprising the compound of  claim 5 , or a polycrystal, a eutectic or a single-enantiomer X-ray diffraction single crystal thereof, and a pharmaceutically-acceptable carrier.

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